The androgen receptor (AR) signalling pathway remains a key driver of prostate cancer progression despite castrate levels of testosterone in advanced disease. The androgen biosynthesis inhibitor abiraterone and the anti-androgen enzalutamide have been shown to prolong survival in randomized clinical trials both pre-and post-docetaxel chemotherapy and are now in routine clinical use. With the use of these drugs and other novel survival-prolonging therapeutics, patients with advanced prostate cancer are now living longer with better quality of life. This article will review pre-clinical and clinical data for AR-targeting therapeutics for advanced prostate cancer with a focus on mechanisms of resistance and future directions for research.
Trial registration: ClinicalTrials.gov NCT01650194.